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US 2021/0079013 A1Published application
Heterobicyclic Carboxylic Acids and Salts Thereof
AssigneesShenzhen Ionova Life Science Co., Ltd., Foshan Ionova Biotherapeutics Co., Inc.
InventorsGang Zhou, Yongkui Sun, Zhaoyin Wang
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Abstract
The present invention provides pharmaceutically acceptable salts of compounds of Formula I that are potent EP4 receptor antagonists and can be used for treating cancer or inflammatory diseases alone or in combination with antibody therapy, radiation therapy, anti-metabolite chemotherapy to a subject in need thereof.
Claims24
A pharmaceutically acceptable salt of a compound of Formula 1,
- wherein:
- R1 and R2 are independently selected from the group consisting of hydrogen, halo, C1-6 alkyl, C1-6 cycloalkyl, C1-6 fluorocycloalkyl, and C1-6 fluoroalkyl;
- or, R1 and R2, together with the carbon atom to which they are both attached, form a three- to six-membered carbocyclic group which is optionally substituted with Rc, or form a three- to six-membered heterocyclic group which contains one or two heteroatom(s) each independently selected from the group consisting of S, O, and NRb;
- each Rb is independently selected from the group consisting of hydrogen, halo, C1-6 alkyl, C1-6 cycloalkyl, C1-6 fluorocycloalkyl, C1-6 fluoroalkyl, aryl, heteroaryl, —C(O)—C1-6 alkyl, —C(O)-aryl, —S(O)2-alkyl, and —S(O)2-aryl;
- Y is O or S;
- X is a bond, ═CH—, CH2, O, or S;
- Ar1 and Ar2 are each independently selected from the group consisting of C3-6 cycloalkyl, aryl, heteroaryl and heterocyclyl, or a fused analog of C3-6 cycloalkyl, aryl, heteroaryl, and heterocyclyl, and Ar1 and Ar2 are each optionally substituted with one to three Rc groups;
- each Rc is independently selected from the group consisting of halo, C1-6 alkyl, C1-6 cycloalkyl, C1-6 fluorocycloalkyl, and C1-6 fluoroalkyl;
- Ra is —CO2H, —CO2M, —C(O)NHS(O)2Raa, or
- Raa is C1-6 alkyl, C1-6 haloalkyl, C1-6 cycloalkyl, C1-6 cyclohaloalkyl, aryl, or heteroaryl;
- M is a pharmaceutically acceptable salt or an ester prodrug group;
- is a 6,6- 5,5- 5,6- or 6,5-bicyclic group.
9 more elements
Dependencies are inferred from the claim text.